Multi-layered pill or tablet with indicating lamination



Jana. 12, 1960 c. a. MODERMOTT MULTI-LAYERED PILL OR TABLET WITH INDICATING LAMINATION Filed April 16, 1957 INVENTOR. (Juan: 5. fiakmm- MllL'II-LAYERED PILL R TABLET WITH INDICATING LAMINATION Charles B. McDermott, New York, N.Y., assignor to Sterling Drug Inc., New York, N.Y., a corporation of Delaware 1 Application April 16, 1957, Serial No. 653,247

scnims. (Cl.16782) This application is a continuation-in-part of my prior application S'erialNo. 449,732, filed August 13, 1954, now

abandoned. v

This invention relates to a rnulti-layere'd pill or tablet particularly adapted for medicinal use and having a medicinal core and a signal layer or lamination, said sig- Patented Jan 12 ,,19 60 a sweet component. Such bland or sweet flavors are apt to be confused by the patient with sugar coatings which are often necessary in any particular tablet formulation. The acidic fruit flavors are readily discernible even in the presence of a sweetening agent, and it may in some instances be desired to enhance the acidic character of the 5 fruit flavors by incorporating a fruit acid such as citric or tartaric acid.

In other words, the tablet is intended to be retained by the patient in his mouth for absorption of the outer layer 10 which is a medicament, until the tasteindicating signal layer 12'is exposed. This serves as a signal for nal lamination having an outer medicinal layer which is v soluble in the patients mouth, to the end that the pill is held by the patient for absorption of theouter layer until the signal layer is exposed, the signal layer serving as an indication to the patient to swallow the tablet to obtain the benefits of'gastro-intestinal absorption of the medicament within the pill or tablet; and the provision of a pill or tablet as above described including a plurality of lay-v ers, so that diiferent or succeeding spaced dosages may be adr'ninistered,the core being covered by an enteric the patient to swallow the tablet. However, the outermost layer may contain the taste signal and oral medicament, which when gone, then gives the signal to the patient to swallow the pill.

release the contained medicine at .a definite point in the travel of the-pill through the gastro-intestinal tract.

coating, and in the event that a plurality of layers of n medicament are provided within the taste-indicating signal layer, such multiple layers may each be covered enterically.

Further objects of the invention include the provision of the signal layer at the. exterior of the tablet, so that. when the taste sensation thereof ceases, the signal is then given; and also, the signal material may be mixed in with a medicament either at the exterior of the tablet or in an inner layer.

Other objects and advantages of the invention will appear hereinafter.

Reference is to be had to the accompanying drawings, in which I Fig. l is a cross section'through a pill or tablet made according to the present invention; and

Fig. 2 isa modification thereof.

The present invention provides a means for dosing a patient with at least two separate medicaments, one of which is to be adsorbed in the mouth and the other in the gastro-intestinal tract, with a relatively increased exactness of absorption time for the orally applied medica- .ment, so that the patient will not tend to hold the pill or tablet for too long or too short a time in the mouth and also providing a means for avoiding variation of the oral dosage due to lack of or more vigorous sucking on the tablet than might otherwise be the case.

To this end, the tablet is provided with an outer, preferably medicinal, coating 10 which is readily dissolved in the mouth, and directly under this layer there is a taste-indicating signal layer 12, so that the patient will know at once when the outer layer is gone and that the time has come to swallow the pill or tablet.

The taste-indicating signal layer 12 contains a distinctive tasting material, as for instance an acidic or other highly distinctive non-sweet flavoring such as fruit flavors in general-orange, lemon, lime, cherry, pineapple, mint, etc., or it might even contain a bitter or alkaloidal flavoring such as quinine. Naturally a more pleasant or attractive flavoring would be better than a bitter one in most cases. The blander flavors such as vanilla, chocolate, licorice, etc. have a less-distinctive flavor and even The invention may of course be continued to provide other layers of medicament, enteric coatings 18, and finally the core 20 of the final dosage to be given the patient.

The invention is further illustrated by the following examples without, however, being limited thereton Example 1 N-isopropylarterenol and the delayed action of theoph'yl lin and benzylephedrine could be obtained were pre' pared as follows: i I

A medicament core 20 was prepared in the followin manner:

The following ingredients were weighed out separately,

screenedto 30 mesh, and mixed:

- Parts Benzylephedrine 32.4 Theophyllin 129.6

Phenobarbital" 8.1, Starch 38.8 Talc 14.5. Stearic acid 2.3 Magnesium stearate 0.9

The mixture was slugged, screened to 12 mesh, and pressed on a A concave tablet punch machine. The core was completed by applying three coats of shellac and tale.

A signal mixture for use in layer 12 was prepared from the following ingredients:

Parts Citric acid 5 Orange flavor 5 Sucrose 530 Finally, the tablets were coated with 70% sucrose aqueous syrup until the tablets were smooth and well-covered, after which they were finished with a carnauba wax solution .in conventional manner.

Example 2 Parts Pentaerithrytol tetranitrate 2800 Starch 500 Dicalcium phosphate 9-14 Alginic acid 86 Stearic acid 100 The ingredients were screened to 30 mesh, mixed, slugged, ground to 12 mesh, and pressed into tablets using a. concave punch. The resulting tablets were given three coats of shellac, dusted with talc, and then a signal layer 12 was applied using an orange flavor in the same manner as in Example 1.

Thereafter the tablets were sugar-coated with 70% sucrose solution and then dusted after moistening with gelatin until by assay the tablets contained a therapeutic dose ofnitroglycerine, the nitroglycerine, being a detonation-sensitive liquid, being dusted safely as in the form of a 10% admixture on an inert solid diluent such as lactose. Thereafter the tablets were sugar-coated and polished with carnauba wax in-conventional manner.

Instead of orange flavor and citric acid as the signal component, other signal components also used included mint and lemon flavors. In any event, the signal material should be distinctive and of such character as to convey a definite signal to the patient to swallow the tablet or pill, as distinguished from the ordinary sugar or chocolate coating used merely to make the taste pleasant, although sugar or the like may, if desired, be combined with the distinctive signal material within the scope of my invention.

Instead of providing the signal (1) as a layer between the outer medicament layer and the core, the signal may appear (2) at the exterior, or (3) may be mixed through? out the outer medicament layer, so that then the disappearance of the taste sensation serves as a signal for the patient to swallow the tablet. This is shown in Fig. 2 wherein 22 indicates the core of medicament, 24 an interposed layer of medicament or coating, and 26 the outermost layer which is the signal material itself, or a medicated layer containing the signal material in mixture therewith. In this case, the disappearance of the taste sensation signals the patient to swallow the tablet, whereas if the signal layer is interior, as at '12, the appearance thereof is the sign. Also, of course, the interior 4 i 7 signal layer 12 can be mixed with a. medicament, and in this invention it is to be understood that the term "signal layer may include medicament or not as circumstances call for.- e

Itiis pointed out that it is very doubtful that a sugar layer per se would serve as a signal to a patient, while a flavored layer immediately informs the patient that the sublingual dosage has been dissolved from the tablet. Further confusion may develop if the signal layer itself is not definite and sharp, and therefore a sweet layer cannot make as efiective a signal layer as contemplated by the foregoing.

Having thus described my invention and the advantages thereof, I do not wish to be limited to the details herein disclosed, otherwise than as set forth in the claims, but what I claim is:

l. A medicament tablet comprising an external layer of tasteless therapeutic material releasable in the mouth for prompt therapeutic action, a signal layer interior of said tasteless external layer and completely surrounded by said external layer, said interior layer containing a signal material sharp to the taste and serving to signal for swallowing of the tablet after the therapeutic material in the external layer has been released, and a core of therapeutic material absor'bable in the gastrointestinal tract for delayed therapeutic action, said core being completely enclosed by said interior layer.

2. A medicament tablet composed of a core containing a slow-acting bronchodilator drug, a layer of acidic material completely surrounding said core and serving, on exposure in the mouth, as a signal to swallow the tablet, and a tasteless layer exterior of said layer of acidic material and completely surrounding it and containing a bronchodilator drug releasable in the mouth and promptly elfective thereafter.

3. A medicament tablet composed of a core containing a slow-acting vasodilator drug, a layer of acidic ma terial completely surrounding said core and serving, on exposure in the mouth, as a signal to swallow the tablet, and a tasteless layer exterior of said layer of acidic material and completely surrounding it and containing a vasodilator drug releasable in the mouth and promptly effective thereafter.

References Cited in the file of this patent FOREIGN PATENTS Great Britain Apr. 9, 1952 OTHER REFERENCES Co., Easton, Pa, 1948, pp. 958-68.

wary, v 

1. A MEDICAMENT TABLET COMPRISING AN EXTERNAL LAYER OF TASTELESS THERAPEUTIC MATERIAL RELEASABLE IN THE MOUTH FOR PROMPT THERAPEUTIC ACTION, A SIGNAL LAYER INTERIOR OF SAID TASTELES EXTERNAL LAYER AND COMPLETELY SURROUNDED BY SAID EXTERNAL LAYER SAID INTERIOR LAYER CONTAINING A SIGNAL MATERIAL SHARP TO THE TASTE AND SERVING TO SIGNAL FOR SWALLOWING OF THE TABLET AFTER THE THERAPEUTIC MATERIAL IN THE EXTERNAL LAYER HAS BEEN RELEASED, AND A CORE OF THERAPEUTIC MATERIAL ABSORBABLE IN THE GASTROINTESTINAL TRACT FOR DELAYED THERAPEUTIC ACTION, SAID CORE BEING COMPLETELY ENCLOSED BY SAID INTERIOR LAYER. 